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dimethylation

" in MedChemExpress (MCE) Product Catalog:

37

Inhibitors & Agonists

18

Peptides

4

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114965
    TP-064
    Maximum Cited Publications
    8 Publications Verification

    Histone Methyltransferase Inflammation/Immunology Cancer
    TP-064, a chemical probe, is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities .
    TP-064
  • HY-134124

    Reactive Oxygen Species (ROS) Metabolic Disease
    Glutathione ethyl ester is a cell-permeable GSH donor and provides an efficient supply of GSH to the oocyte. Glutathione ethyl ester shows positive effect on the in vitro production of embryos by enhancement of the antioxidative defense .
    Glutathione ethyl ester
  • HY-P10272

    PTG-300

    Ferroportin Others
    Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .
    Rusfertide
  • HY-A0248A
    Polymyxin B1
    1 Publications Verification

    Bacterial Infection
    Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .
    Polymyxin B1
  • HY-159099

    Molecular Glues Histone Acetyltransferase Cardiovascular Disease
    WIZ degrader 9 is an orally active molecular glue degrader of the WIZ transcription factor. As a molecular glue, WIZ degrader 9 recruits WIZ to the cereblon E3 ubiquitin ligase complex via its ZF7 domain, driving proteasome-dependent degradation of WIZ. WIZ degrader 9 induces hemoglobin production, reduces the level of H3K9 dimethylation across the whole genome and at the β-globin locus, upregulates the transcription of γ-globin and BGLT3, and increases the level of histone H3K9 acetylation in the promoter region of HBG1/2. WIZ degrader 9 effectively induces fetal hemoglobin production in both mice and cynomolgus monkeys. WIZ degrader 9 can be used for research on sickle cell disease .
    WIZ degrader 9
  • HY-159098

    Molecular Glues PROTACs Histone Acetyltransferase Cardiovascular Disease
    dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
    dWIZ-1
  • HY-P1108A
    Astressin 2B TFA
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B TFA
  • HY-P1108
    Astressin 2B
    1 Publications Verification

    CRFR Neurological Disease Inflammation/Immunology
    Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
    Astressin 2B
  • HY-100360
    MS049
    1 Publications Verification

    Histone Methyltransferase Cancer
    MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
    MS049
  • HY-162308

    Histone Methyltransferase Apoptosis Cancer
    NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
    NSD-IN-3
  • HY-44062

    Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
    G9a-IN-1
  • HY-178825

    PROTACs Histone Demethylase Apoptosis Cancer
    LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer .
    LD-110
  • HY-P10143

    Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt

    MMP Others
    MMP-2/MMP-9 Substrate (Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt) is a synthetic chromogenic polypeptide substrate whose core structure mimics the cleavage sites of MMP-2 and MMP-9 (gelatinase A and B) in collagen. After being hydrolyzed by collagenase, MMP-2/MMP-9 Substrate reacts with 4,4'-dithiodipyridine or Ellman's Reagent via its thiol fragment to produce a product with ultraviolet absorption properties .
    MMP-2/MMP-9 Substrate
  • HY-A0248AS

    Isotope-Labeled Compounds Bacterial Infection
    Polymyxin B1-d7 TFA is the deuterium labeled Polymyxin B1 TFA (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .
    Polymyxin B1-d7 TFA
  • HY-101520A

    Histone Methyltransferase Cancer
    Dot1L-IN-1 TFA is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 TFA potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
    Dot1L-IN-1 TFA
  • HY-172614

    RK-552

    Histone Methyltransferase Apoptosis Cancer
    RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
    RK-0080552
  • HY-P10563

    BHV-1100

    CD38 Cancer
    Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .
    Noraramtide
  • HY-P3066

    d(CH2)5Tyr(Et)VAVP

    Vasopressin Receptor Metabolic Disease
    SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
    SKF 100398
  • HY-101520

    Histone Methyltransferase Cancer
    Dot1L-IN-1 is a highly potent and selective Dot1L inhibitor with a Ki of 2 pM and an IC50 of <0.1 nM. Dot1L-IN-1 potently suppresses H3K79 dimethylation (IC50=3 nM), as well as the activity of the HoxA9 promoter (IC50=17 nM) in HeLa and Molm-13 cells, respectively .
    Dot1L-IN-1
  • HY-P4308

    Prolyl Endopeptidase (PREP) Neurological Disease
    Z-Pro-Pro-aldehyde-dimethyl acetal is a potent inhibitor of prolyl endopeptidase (PREP), a cytoplasmic serine endoprotease (IC50= 12 nM). Z-Pro-Pro-aldehyde-dimethyl acetal plays an important role in cognitive dysfunction in aging and neurodegenerative diseases including Alzheimer's disease .
    Z-Pro-Pro-aldehyde-dimethyl acetal
  • HY-P10828

    Virus Protease Infection Inflammation/Immunology
    MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .
    MAPI
  • HY-P6053

    Opioid Receptor Neurological Disease
    KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect .
    KK-103
  • HY-116971

    Histone Methyltransferase Apoptosis Cancer
    DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .
    DCG066
  • HY-100360A

    Histone Methyltransferase Cancer
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
    MS049 dihydrochloride
  • HY-168083

    Histone Methyltransferase Cancer
    Dot1L-IN-9 (Compound 12) is a DOT1L inhibitor (IC50: 125 nM). Dot1L-IN-9 reduces H3K79 dimethylation. Dot1L-IN-9 can be used for anti-leukemia research .
    Dot1L-IN-9
  • HY-168497

    Histone Methyltransferase Cancer
    C-MS023 is a photo-activatable MS023 (HY-19615) prodrug, achieving spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. C-MS023 inhibits PRMT6 mediated asymmetric dimethylation of H3 arginine 2 (H3R2me2a), with an estimate IC50 of 0.2224 μM. The photolysis of C-MS023 could be triggered by visible light irradiation at 420 nm, thereby liberating MS023 for effective downregulation of histone arginine asymmetric dimethylation and DNA replication-related transcriptomic activities .
    C-MS023
  • HY-P2592

    Cholecystokinin Receptor Others
    Ro 23-7014 is an appetite suppressant. Ro 23-7014 is an analog of cholecystokinin (CCK-7) .
    Ro 23-7014
  • HY-125628

    Endogenous Metabolite Infection
    Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .
    Kahalalide A
  • HY-186091

    Amino Acid Derivatives Others
    AcdK is a non-natural amino acid and a precursor of allysine. AcdK allows site-specific incorporation into target proteins in E. coli via the amber suppression strategy. AcdK enables site-specific lysine dimethylation or monomethylation modification of target proteins. AcdK can synthesize site-specific lysine-methylated variants of histone H3 and p53, which is applicable for investigating the substrate specificity and catalytic function of epigenetic enzymes .
    AcdK
  • HY-E71200A

    Biochemical Assay Reagents Others
    KsgA introduces the most highly conserved ribosomal RNA modification, the dimethylation of adenine1518 and adenine1519 in 16S rRNA. Strains lacking the methylase are resistant to kasugamycin.
    16S rRNA (adenine1518-N6/adenine1519-N6)-Dimethyltransferase
  • HY-178825B

    PROTACs Histone Demethylase Apoptosis Cancer
    LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 trihydrochloride promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 trihydrochloride inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 trihydrochloride can be used for the study of esophagus squamous cancer .
    LD-110 trihydrochloride
  • HY-100360R

    Histone Methyltransferase Reference Standards Cancer
    MS049 (Standard) is the analytical standard of MS049 (HY-100360). This product is intended for research and analytical applications. MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
    MS049 (Standard)
  • HY-178825A

    Histone Demethylase Apoptosis PROTACs Cancer
    LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 triTFA promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 triTFA inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 triTFA can be used for the study of esophagus squamous cancer .
    LD-110 triTFA
  • HY-182275

    PROTACs Histone Methyltransferase Cancer
    PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
    PROTAC PRMT1 degrader-1
  • HY-P11673

    GLP Receptor Metabolic Disease
    Zabopegdutide is a glucagon and glucagon-like peptide 1 (GLP-1) receptor agonist. Zabopegdutide can be used for the study of obesity .
    Zabopegdutide
  • HY-123153

    Isocitrate Dehydrogenase (IDH) Cancer
    GSK990 is an inactive mutant IDH1 inhibitor with no significant inhibitory activity against wild-type or mutant IDH1/IDH2 enzymes. In experiments, GSK990 can serve as an inactive negative control for the IDH1 inhibitor GSK321 (HY-18948). GSK990 is applicable to the research of acute myeloid leukemia .
    GSK990
  • HY-A0248AS1

    Isotope-Labeled Compounds Bacterial Infection
    Polymyxin B1-D-Leu-d7 TFA is the deuterium labeled Polymyxin B1 (HY-A0248A). Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment .
    Polymyxin B1-D-Leu-d7 TFA

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